CLEFMA

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

CLEFMA 

CLEFMA 是一种具有抗肿瘤活性的姜黄素。CLEFMA 抑制肿瘤生长与 NF-κB 调节的抗炎和抗转移作用有关。

CLEFMA

CLEFMA Chemical Structure

CAS No. : 1246964-32-8

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生物活性

CLEFMA is a curcuminoid with antitumor activity. CLEFMA inhibits tumor growth is associated with NF-κB-regulated anti-inflammatory and anti-metastatic effects[1][2].

体外研究
(In Vitro)

CLEFMA (1-100 μM; 24-72 h) has anti-proliferative activity[1].
CLEFMA inhibits the viability of H441 and A549 cells, with IC50s of 6.4 and 8.9 μM, respectively[2].
CLEFMA (5-10 μM; 24 h) induces apoptosis in H441 and A549 cells[2].
CLEFMA (1 and 10 μM; 24 h) induces autophagic death in H441 cells[1].
CLEFMA (1-20 μM) reduces the DNA-binding activity of NF-κB in H441 cells in a dose-dependent manner[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: PANC-1, MiaPaCa-2, PC-3 and H441 cells
Concentration: 1, 10, 25, 100 μM
Incubation Time: 24, 48, 72 h
Result: Inhibits cells proliferation in a dose-dependent manner.

体内研究
(In Vivo)

CLEFMA (0.2-0.4 mg/kg; i.p. daily for 4 weeks) inhibits tumor growth and suppresses the uptake of FDG in tumor tissue in a xenograft mouse model[2].
CLEFMA (0.2-0.4 mg/kg; i.p. daily for 4 weeks) down-regulates the expression of anti-apoptotic markers cIAP1, Bcl-xL, Bcl-2 and survivin, and induces the cleavage of pro-apoptotic protein BID and the expression of pro-apoptotic BAX in tumor tissue[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male athymic nu/nu mice (4 weeks old) are injected H441 cells[2]
Dosage: 0.2, 0.4 mg/kg
Administration: I.p. daily for 4 weeks
Result: Inhibited tumor growth up to 96% tumor at dose of 0.4 mg/kg.

分子量

442.29

Formula

C23H17Cl2NO4

CAS 号

1246964-32-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Lagisetty P, et, al. CLEFMA-an anti-proliferative curcuminoid from structure-activity relationship studies on 3,5-bis(benzylidene)-4-piperidones. Bioorg Med Chem. 2010 Aug 15; 18(16):6109-20.

    [2]. Yadav VR, et, al. Preclinical evaluation of 4-[3,5-bis(2-chlorobenzylidene)-4-oxo-piperidine-1-yl]-4-oxo-2-butenoic acid, in a mouse model of lung cancer xenograft. Br J Pharmacol. 2013 Dec; 170(7): 1436-48.

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